AR085549A1 - TRIAZOLIL PIPERAZINA AND TRIAZOLIL PIPERIDINA DERIVATIVES REPLACED AS MODULATORS OF g SECRETASE - Google Patents

TRIAZOLIL PIPERAZINA AND TRIAZOLIL PIPERIDINA DERIVATIVES REPLACED AS MODULATORS OF g SECRETASE

Info

Publication number
AR085549A1
AR085549A1 ARP120100976A ARP120100976A AR085549A1 AR 085549 A1 AR085549 A1 AR 085549A1 AR P120100976 A ARP120100976 A AR P120100976A AR P120100976 A ARP120100976 A AR P120100976A AR 085549 A1 AR085549 A1 AR 085549A1
Authority
AR
Argentina
Prior art keywords
triazolil
alkyl
hydrogen
compounds
secretase
Prior art date
Application number
ARP120100976A
Other languages
Spanish (es)
Original Assignee
Janssen Pharmaceuticals Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Janssen Pharmaceuticals Inc filed Critical Janssen Pharmaceuticals Inc
Publication of AR085549A1 publication Critical patent/AR085549A1/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D249/14—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biomedical Technology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Los compuestos de acuerdo con la presente son útiles como moduladores de g secretasa. Además se refiere a procesos para preparar tales compuestos, composiciones farmacéuticas que comprenden dichos compuestos como un ingrediente activo así como también el uso de dichos compuestos como un medicamento.Reivindicación 1: Un compuesto de fórmula (1) o una forma estereoisomérica del mismo, donde R1 y R2 se seleccionan de manera independiente del grupo compuesto por hidrógeno, halo, alquilo C1-4, alquiloxi C1-4, alquilo C1-4 sustituido con uno o más sustituyentes halo, y alquiloxi C1-4 sustituido con uno o más sustituyentes halo; L1 es NR6, O, carbonilo o un enlace covalente; donde R6 es hidrógeno o alquilo C1-4; R3 representa alquilo C1-4; R4a y R4b se seleccionan de manera independiente del grupo compuesto por hidrógeno y alquilo C1-4; X es N o CH; L2 es; O, CH2 o un enlace covalente; siempre que cuando L2 sea O, entonces X es CH; R5 es hidrógeno o alquilo C1-4; Y1 es CH o N; Y2 es CR7 o N; donde R7 representa H o alquiloxi C1-4; o una sal de adición o solvato farmacéuticamente aceptable del mismo.The compounds according to the present are useful as g secretase modulators. It also refers to processes for preparing such compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament. Claim 1: A compound of formula (1) or a stereoisomeric form thereof, wherein R1 and R2 are independently selected from the group consisting of hydrogen, halo, C1-4 alkyl, C1-4 alkyloxy, C1-4 alkyl substituted with one or more halo substituents, and C1-4 alkyloxy substituted with one or more halo substituents ; L1 is NR6, O, carbonyl or a covalent bond; where R6 is hydrogen or C1-4 alkyl; R3 represents C1-4 alkyl; R4a and R4b are independently selected from the group consisting of hydrogen and C1-4 alkyl; X is N or CH; L2 is; O, CH2 or a covalent bond; provided that when L2 is O, then X is CH; R5 is hydrogen or C1-4 alkyl; Y1 is CH or N; Y2 is CR7 or N; where R7 represents H or C1-4 alkyloxy; or a pharmaceutically acceptable addition salt or solvate thereof.

ARP120100976A 2011-03-24 2012-03-23 TRIAZOLIL PIPERAZINA AND TRIAZOLIL PIPERIDINA DERIVATIVES REPLACED AS MODULATORS OF g SECRETASE AR085549A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP11159639 2011-03-24

Publications (1)

Publication Number Publication Date
AR085549A1 true AR085549A1 (en) 2013-10-09

Family

ID=43952127

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP120100976A AR085549A1 (en) 2011-03-24 2012-03-23 TRIAZOLIL PIPERAZINA AND TRIAZOLIL PIPERIDINA DERIVATIVES REPLACED AS MODULATORS OF g SECRETASE

Country Status (12)

Country Link
US (1) US8987276B2 (en)
EP (1) EP2688874B1 (en)
JP (1) JP2014508794A (en)
KR (1) KR20140047032A (en)
CN (1) CN103502225B (en)
AR (1) AR085549A1 (en)
AU (1) AU2012230348A1 (en)
BR (1) BR112013023984A2 (en)
CA (1) CA2827969A1 (en)
ES (1) ES2536442T3 (en)
MX (1) MX2013010970A (en)
WO (1) WO2012126984A1 (en)

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Also Published As

Publication number Publication date
ES2536442T3 (en) 2015-05-25
AU2012230348A1 (en) 2013-08-29
MX2013010970A (en) 2013-10-17
CN103502225B (en) 2015-11-25
AU2012230348A8 (en) 2013-09-05
KR20140047032A (en) 2014-04-21
CN103502225A (en) 2014-01-08
EP2688874B1 (en) 2015-03-04
BR112013023984A2 (en) 2016-09-13
CA2827969A1 (en) 2012-09-27
JP2014508794A (en) 2014-04-10
US8987276B2 (en) 2015-03-24
US20140011816A1 (en) 2014-01-09
EP2688874A1 (en) 2014-01-29
WO2012126984A1 (en) 2012-09-27

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